High-throughput crystallization:: polymorphs, salts, co-crystals and solvates of phan-naceutical solids

被引:551
作者
Monissette, SL
Almarsson, Ö
Peterson, ML
Remenar, JF
Read, MJ
Lemmo, AV
Ellis, S
Cima, MJ
Gardner, CR
机构
[1] TransForm Pharmaceut Inc, Lexington, MA 02421 USA
[2] MIT, Dept Mat Sci & Engn, Cambridge, MA 02139 USA
关键词
high-throughput; crystallization; polymorph; solvate; salt; co-crystal;
D O I
10.1016/j.addr.2003.10.020
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The concepts of high-throughput (HT) screening and combinatorial synthesis have been integrated into the pharmaceutical discovery process, but are not yet commonplace in the pharmaceutical development arena. Emerging strategies to speed pharmaceutical development and capture solid form diversity of pharmaceutical substances have resulted in the emergence of HT crystallization technologies. The primary type of diversity often refers to polymorphs, which are different crystal forms of the same chemical composition. However, diverse salt forms, co-crystals, hydrates and solvates are also amenable to study in HT crystallization systems. The impact of form diversity encompasses issues of stability and bioavailability, as well as development considerations such as process definition, formulation design, patent protection and regulatory control. This review highlights the opportunities and challenges of HT crystallization technologies as they apply to pharmaceutical research and development. (C) 2003 Elsevier B.V. All rights reserved.
引用
收藏
页码:275 / 300
页数:26
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